99m Tc-Radiolabeled TPGS Nanomicelles Outperform 99m Tc-Sestamibi as Breast Cancer Imaging Agent

NUÑEZ, MARIEL; TESAN, FIORELLA C.; SALGUEIRO, MARÍA J.; MEDINA, VANINA A.; NUÑEZ, MARIEL; TESAN, FIORELLA C.; SALGUEIRO, MARÍA J.; MEDINA, VANINA A.; NICOUD, MELISA B.; CHIAPPETTA, DIEGO A.; NICOUD, MELISA B.; CHIAPPETTA, DIEGO A.

CONTRAST MEDIA & MOLECULAR IMAGING

JOHN WILEY & SONS LTD

Año: 2019 vol. 2019 p. 1 - 9

1555-4309

D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) is a Food and Drug Administration (FDA) approved biomaterial thatcan form nanosized micelles in aqueous solution. TPGS micelles stand as an interesting system to perform drug delivery as theycan carry lipophilic drugs and overcome P glycoprotein e?ux as well. ?erefore, TPGS micelles combined with other copolymershave been reported in many cancer research studies as a carrier for therapeutic drugs. ?eir ability to reach tumoral tissue can alsobe exploited to develop imaging agents with diagnostic application. A radiolabeling method with 99mTc for TPGS nanosizedmicelles and their biodistribution in a healthy animal model as well as their pharmacokinetics and radiolabeling stability in vivowas previously reported. ?e aim of this work was to evaluate the performance of this radioactive probe as a diagnostic imagingagent compared to routinely available SPECTradiopharmaceutical, 99mTc-sestamibi. A small eld of view gamma camera was usedfor scintigraphy studies using radiolabeled TPGS micelles in two animal models of breast cancer: syngeneic 4T1 murine cell line(injected in BALB/c mice) and chemically NMU-induced (Sprague-Dawley rats). Ex vivo radioactivity accumulation in organs ofinterest was measured by a solid scintillation counter, and a semiquantitative analysis was performed over acquired images as well.Results showed an absence of tumoral visualization in 4T1 model for both radioactive probes by gamma camera imaging. On thecontrary, NMU-induced tumors had a clear tumor visualization by scintigraphy. A higher tumor/background ratio and morehomogeneous uptake were found for radiolabeled TPGS micelles compared to 99mTc-sestamibi. In conclusion, 99mTc-radiolabeledTPGS micelles might be a potential SPECT imaging probe for diagnostic purposes.